Dental preparations containing orotic acid

ABSTRACT

A dental preparation for the care of the mouth which exerts a refreshing and stimulating action on the mucous membranes of the mouth and the gum contains uracil-4-carboxylic acid and/or its inorganic and organic salts, optionally with a solubilizer.

United States Patent Harth et a. 1 Sept. 5, 1972 [54] DENTALPREPARATIONS [56] References Cited CONTAINING OROTIIC [It/[CID K I RaOTHER PUBLICATIONS lm t Hart ar u [72] Inventors g g i gg Helm Hamann,Drug and Cosmetic Industry, Vol. 68, pp.

Wagner, 1m Erlich an of Germany 174, I75 and 24 9- 253, Feb. 1951 Eichelet al., Science, Vol. 166, pp. 1424- 1428, Dec. [73] Assignee:Blendax-Werke R. Schneider & Co., 1969 Germany Chemical Abstracts 1 Vol.59, entry l4222c, I963 [22] Filed: May 12, 1970 Chemical Abstracts (2),Vol. 67, entry 1943c, 1967 [21] Appl' 36,677 Primary Examiner-Richard L.Ruff Attorney-Arthur G. Connolly and Rudolf E. l-lutz [30] ForeignApplication Priority Data May 29, 1969 Germany ..P 19 27 425.0 [57]ABSTRACT A dental preparation for the care of the month which il exertsa refreshing and stimulating action on the mm 58 Field oi Searc ii151735; 54; 167/93 Cous membranes of the mouth and the gum containsuracil-4-carboxylic acid and/or its inorganic and organic salts,optionally with a solubilizer.

3 Claims, No Drawings DENTAL PREPARATIONS CONTAINING OROTIC ACID Thisinvention is related to dental preparations for the care of the mouth,such as mouth washes, toothpastes, tooth powders, chewing gum,teeth-cleaning and chewing tablets or dragees, which exert a refreshingand stimulating action on the mucus membranes of the mouth and on thegum.

Uracil-4-carboxylic acid or 2,6-dioxo-l,2,3,6-tetrahydropyrimidine-4-carboxylic acid, also known by the trivial nameorotic acid, is used as an anticholesterinaemic agent, liver-therapeuticagent and anti-arthritic agent in pharmacy. The present inventionprovides a material for the care of the mouth, containinguracil-4-carboxylic acid and/or one or more salts thereof together withone or more conventional constituents of mouth preparations ashereinafter defined.

The invention is based on the observation that uracil- 4-carboxylic acidexerts a vessel-activating blood perfusion-promoting action on the gumand is therefore excellently suited for use in materials for the care ofthe mouth.

When the material for the care of the mouth is present in aqueousmedium, a solubilizing agent for uracil-4-carboxylic acid, such as oneor more aminoacids, especially glycine and/or lysine or methylglucaminemay also be present with adventage.

If it is desired that the materials for the care of the mouth shall havean additional caries-prophylactic action, the incorporation of one ormore of numerous fluorine compounds is advisable, such as for examplesodium fluoride, potassium fluoride, ammonium fluoride, lithiumfluoride, aluminum fluoride, magnesium fluoride, palladium fluoride,zirconium fluoride, tin fluoride, iron fluoride, alkalifluorozirconates, tin fluorozirconate, fluorostannites, fluoroborates oralkali monofluorophosphates. Organic fluorine compounds such as aminehydrofluorides may also be present. Mixtures of the different fluorinecompounds may be used. Furthermore, agents which dissolve dental tartarand remove dental fur, such as complex-forming agents, for exampleethylene diaminotetraacetic acid and its alkali salts, or variouswater-soluble polyphosphonic acid compounds, such as for examplel-hydroxyethylidener l-hydroxypropylidene-disphosphonic acid, and alsoenzymes, especially carbohydrases such as amylases, dextranases,lysozyme, and proteases, such as pepsin, trypsin, chymotrypsin, papaine,bromeline, and bacterial or fungal proteases, lipases and mixtures ofsuch enzymes, such as are present for example in pancreatin, may also beused in the preparations for the care of the mouth, according to theinvention.

These preparations may additionally contain various vitamins, forexample of the vitamin B6- or Bl2-complex, and also antibiotics andother bactericidally active substances, and preservatives. By way ofexample, there may be mentioned various phenols, such ashexachlorophene, or the lower esters of p-hydroxybenzoic acid and thevarious quaternary ammonium compounds.

lf the dental preparations according to the invention are to be in theform of toothpastes or tooth powders, the incorporation of polishingsubstances and optionally of fillers is appropriate. Substances whichserve this purpose are, for example, dicalcium phosphate and/or itsdihydrate, calcium carbonate, insoluble alkali metaphosphate, tricalciumphosphate, calcium pyrophosphate, aluminum oxide and its trihydrate,kaolin, silicon dioxide of various particle sizes, zirconium andaluminum silicate, pulverulent plastics, such as melamime-formaldehydeor urea-formaldehyde resins, polymethyl methacrylate, polyamide powdersand polyvinyl chloride, and also mixtures of these substances.

Carboxymethylc'ellulose, alginates, tragacanth, polyacrylic acid and itsalkali salts, polyvinylpyrrolidone and various vegetable mucilagesareused as binders and thickeners in toothpastes. Moisturizing agentsinclude, for example, glycerol, sorbitol and other sugar alcohols, andalso various aliphatic alkanediols.

In addition to the aroma substances and flavoring substances which arecustomary in dental preparations and materials for the care of themouth, it is possible, where required, also to incorporate dyestuffs,optical brighteners and small amounts of solvents, such as aliphaticalcohols or chloroform, astringent agents which further intensify theagreeable action of uracil-4- carboxylic acid on the gum, such asaluminum salts, for example aluminum lactate, or zinc salts in lowconcentrations.

It is also possible to incorporate various surface-active substances aswetting agents and foaming agents in the dental preparations accordingto the invention. As such agents there may be mentioned anionicsubstances such as fatty alcohol sulphates, alkylarylsulphonates, olefinsulphonates and fatty acid-protein condensates, cationic substances suchas quaternary ammonium compounds, non-ionic substances such as ethyleneoxide and propylene oxide condensates with alcohols and amines or amineoxides, and also 'amphoteric surface-active substances such as betainesor long-chain alkylamino-carboxylic acids. It is also possible to usemixtures of such substances.

The uracil-4-carboxylic acid (orotic acid) to be used according to theinvention in materials for the care of the mouth, and its organic orinorganic salts, are available as commercial products.Uracil-4-carboxylic acid is present in cows milk and can also beobtained by fermentation of various micro-organisms, and alsosynthetically. The proportion of uracil-4-carboxylic acid in thematerials for the care of the mouth according to the invention is notcritical, just as the pH-value in an aqueous medium is not critical, butthe preferred range is 0.25 5.0 percent by weight of the totalcomposition.

The following examples illustrate the invention; in examples 1-6 thefigures given are percentages by weight.

Carboxymethylcellulose Methyl-p-hydroxybenzoate Uracil-4-carboxylic acidLysine Glycine Aroma substances Sodium saccharin Lauryldimethylamineoxide Water 3.) Toothpaste Dicalciurn phosphate dihydrate Polyvinylchloride powder Polyacrylic acid, sodium salt Sodium monofluorophosphateSodium lauryl-sulphate Uracil-4-carboxylic acid MethylglucamineSorbitol, 60% strength Glycerol, 86% strength Aroma and flavoringsubstances Sodium saccharin Sodium dihydrogen phosphate HexachloropheneWater 4.) Tooth Powder Dicalcium phosphate dihydrate Dicalcium phosphateanhydrous) Cured melamine-formaldehyde condensation productWater-insoluble sodium metaphosphate Sodium lauryl-sulphateUracil-4-carboxylic acid Pancreatin Flavoring and aroma substancesSodium saccharin 5.) Toothpaste in Gel form Silicon dioxide gel(Syloid"63of Grace GmbH,

particle size micron, surface area 830 cmlg Silicon dioxid gel(Syloid"72of Grace GmbH,

particle size 3micron, surface area 370 cm lg Sorbitol, 60% strengthGlycerol, 86% strength Carboxymethylcellulose Uracil4-carboxylic acidGlycine Sodium N-lauroylsarcoside Hexachlorophene Sodium saccharinFlavoring and aroma substances Water We claim: 1. A dentrificepreparation for use in the care of the mouth containing a dentallyacceptable carrier and an active agent in an amount sufficient to exerta vesselactivating blood perfusion promoting action on the gum, saidactive agent being orotic acid.

2. The dentifrice preparation of claim 1 wherein the orotic acid ispresent in an amount of from 0.25-5 percentb Wei ht.

3. X mefi'iod for exerting a vessel-activating. blood perfusionpromoting action on the gum in the mouth comprising contacting the gumwith a dentifrice preparation containing a dentally acceptable carrierand an active agent in an amount sufficient to exert a vessel-activatingblood perfusion promoting action on the gum, said active agent beingorotic acid.

2. The dentifrice preparation of claim 1 wherein the orotic acid ispresent in an amount of from 0.25-5 percent by weight.
 3. A method forexerting a vessel-activating blood perfusion promoting action on the gumin the mouth comprising contacting the gum with a dentifrice preparationcontaining a dentally acceptable carrier and an active agent in anamount sufficient to exert a vessel-activating blood perfusion promotingaction on the gum, said active agent being orotic acid.